clofazimine [Ligand Id: 9184] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1292 (Chlofazimine, Clofazimine, Clofaziminum, Colfazimine, G 30320, G-30320, Lamprene, NSC-141046)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) F 4.54 pIC50 28700 nM IC50 Pharm Res (2003) 20: 537-544 [PMID:12739759]
Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100 B 4.4 pIC50 40000 nM IC50 J Med Chem (2010) 53: 4259-4265 [PMID:20426472]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine in presence of 0.01% Triton B 4.4 pIC50 40000 nM IC50 Eur J Med Chem (2015) 93: 338-348 [PMID:25707014]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 B 5.22 pIC50 6000 nM IC50 J Med Chem (2010) 53: 4259-4265 [PMID:20426472]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine in absence of 0.01% Triton B 5.22 pIC50 6000 nM IC50 Eur J Med Chem (2015) 93: 338-348 [PMID:25707014]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 5.96 pIC50 1100 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 6 pIC50 1000 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 6.22 pIC50 600 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite growth after 72 hrs by parasite lactate dehydrogenase assay F 5.15 pIC50 7020 nM IC50 Bioorg Med Chem (2015) 23: 55-65 [PMID:25497962]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 assessed as inhibition of parasite growth after 72 hrs by parasite lactate dehydrogenase assay F 5.32 pIC50 4820 nM IC50 Bioorg Med Chem (2015) 23: 55-65 [PMID:25497962]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 5.39 pIC50 4100 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]